RT Journal Article SR Electronic T1 Ivermectin: A Positive Allosteric Effector of the α7 Neuronal Nicotinic Acetylcholine Receptor JF Molecular Pharmacology JO Mol Pharmacol FD American Society for Pharmacology and Experimental Therapeutics SP 283 OP 294 DO 10.1124/mol.53.2.283 VO 53 IS 2 A1 Ryoko M. Krause A1 Bruno Buisson A1 Sonia Bertrand A1 Pierre-Jean Corringer A1 Jean-Luc Galzi A1 Jean-Pierre Changeux A1 Daniel Bertrand YR 1998 UL http://molpharm.aspetjournals.org/content/53/2/283.abstract AB We report that preapplication of ivermectin, in the micromolar range, strongly enhances the subsequent acetylcholine-evoked current of the neuronal chick or human α7 nicotinic acetylcholine receptors reconstituted in Xenopus laevis oocytes and K-28 cells. This potentiation does not result from nonspecific Cl−currents. The concomitant increase in apparent affinity and cooperativity of the dose-response curve suggest that ivermectin acts as a positive allosteric effector. This interpretation is supported by the observation of an increase in efficiency of a partial agonist associated with the potentiation and by the differential effect of ivermectin on mutants within the M2 channel domain. Ivermectin effects reveal a novel allosteric site for pharmacological agents on neuronal α7 nicotinic acetylcholine receptors.